Bonde J, Angelo H R, Bødtker S, Svendsen T L, Kampmann J P
Acta Pharmacol Toxicol (Copenh). 1985 Apr;56(4):278-82. doi: 10.1111/j.1600-0773.1985.tb01290.x.
Total body clearance, half-life and volume of distribution of disopyramide (Norpace, Searle G.D.) was measured during a six to eight hour infusion to steady state in twenty four patients with either congestive heart failure or acute myocardial infarction and compared to eleven patients without these diseases. All patients were given a bolus injection of 150 mg disopyramide followed by a continuous infusion of 18-24 mg per hour. Serum concentration of disopyramide and its main dealkylated metabolite were determined by HPLC. The clearance in patients without myocardial infarction or congestive heart failure was 1.71 +/- 0.60 ml/min./kg (mean +/- S.D.), not significantly different from those who had either myocardial infarction, congestive heart failure or both. Half-life was 798 min. in patients without heart failure, not significantly different from the values in the other groups. The ratio between disopyramide and its metabolite varied between 3 to 10. Twenty-six % of the steady state serum concentrations of disopyramide were outside the recommended therapeutic range (2-5 micrograms/ml), but no adverse haemodynamic effects were observed in any of the patients. The suggested dosage regimen of disopyramide seems to result in a satisfactory response.
在24例充血性心力衰竭或急性心肌梗死患者中,在6至8小时输注至稳态期间测量了丙吡胺(诺佩斯,西尔制药公司)的全身清除率、半衰期和分布容积,并与11例无这些疾病的患者进行了比较。所有患者均静脉注射150mg丙吡胺,随后以每小时18 - 24mg的速度持续输注。通过高效液相色谱法测定丙吡胺及其主要去烷基代谢物的血清浓度。无心肌梗死或充血性心力衰竭患者的清除率为1.71±0.60ml/min./kg(平均值±标准差),与患有心肌梗死、充血性心力衰竭或两者兼有的患者无显著差异。无心力衰竭患者的半衰期为798分钟,与其他组的值无显著差异。丙吡胺与其代谢物的比例在3至10之间变化。26%的丙吡胺稳态血清浓度超出推荐治疗范围(2 - 5微克/毫升),但在任何患者中均未观察到不良血流动力学效应。丙吡胺建议的给药方案似乎能产生满意的反应。